Description
An OX1R and OX2R dual antagonist (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors); selectively inhibits OX1R and OX2R over a panel of >170 receptors and enzymes; inhibits orexin A-induced calcium mobilization in CHO cells expressing recombinant human OX1R or OX2R (Kb = 11 nM for both); decreases locomotor activity in rats during the dark cycle at 10 mg/kg; reduces the time spent awake and decreases the latency to SWS1 and SWS2, but not REM sleep, in dogs at 0.5 mg/kg; increases the duration of SWS2, but not SWS1 or REM sleep, in the same model